Abstract:
An optically modulated “turn-on” theranostic prodrug TP1 has
been explored and formulated with biotinylated poly(vinyl alcohol) (biotinPVA)
to obtain desired pharmacokinetics. TP1, consisting of the antineoplastic
camptothecin analogue SN-38, and the fluorescent dye rhodol green have been
covalently conjugated through a disulfide bond. Glutathione triggering the release
of drug and fluorophore has been well established by UV−vis measurements
through mass spectral analysis in physiological conditions. The biocompatible
biotinPVA formulated prodrug (PTP1) showed remarkably higher stability against
blood serum and cell-specific activation in contrast to that of TP1. Significantly,
PTP1 permits monitoring of the delivery and release of well-known topoisomerase
I inhibitor SN-38 by modulating fluorescence signal at λem 550 nm within
intracellular milieus. Moreover, theranostic probe PTP1 exhibited dose-dependent
antiproliferative activity against receptor-positive HeLa cells, whereas it did not
show such an effect against receptor-negative NIH3T3 cells. Finally, the cellspecific
antiproliferative activity of PTP1 via the apoptotic pathway is an efficient approach in cancer theranostics. Thus, futuristic
PTP1 could be a promising agent in which diagnostic and prognostic data will be monitored synergistically
